The present invention relates to new N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ol derivatives, processes for their preparation and pharmaceutical compositions thereof.
Several N.sub.1 -furoyl- and N.sub.1 -benzoyl-N.sub.2 -methyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ol derivatives, which are not within the scope of the present invention, are known in the art and are specifically disclosed in the U.S. Pat. No. 3,998,809 and the German Offenlegungsschriften Nos. 22 21 558 and 23 14 993.
Several N.sub.1 -furoyl- and N.sub.1 -benzoyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ol derivatives according to the present invention fall within the scope of the general formulae which are disclosed in the aforementioned patent and Offenlegungsschriften. Yet, these compounds are not specifically disclosed in these prior art publications. The German Offenlegungsschriften and the U.S. Pat. No. 3,998,809 disclose that the N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ol derivatives are valuable intermediates for the preparation of benzodiazepine- and benzodiazocine derivatives which are pharmacologically effective in influencing the central nervous system and which due to these properties are useful as tranquilizers, sedatives, or anticonvulsive agents. Yet, no independent pharmacological activity of these intermediates has been disclosed.
It is well known in the medical art that the etiology of ulcer-formation is very complex. Pharmaceuticals which so far have been used in the treatment of ulcers each influence only partial aspects of these multiple events. Therefore, only the limited therapeutical success could be obtained (see Blum, Schweiz. Med. Wochenschrift, 106 (1976) p. 1457).
According to Demling (see L. Demling, Klin. Gastroenterologie I, (1973), p. 202), the balance between the various aggressive and defensive factors which act on the mucous membrane is disturbed in the case of ulcer formation in the stomach and intestines. A therapeutical treatment therefore had to be directed towards redressing this balance.
The conventionally used therapeutic methods were directed towards reducing the aggressive agents (hydrochloric acid, pepsin).
Anticholinergic agents, as for example atropine, have not succeeded in ulcer-therapy, because of their side effects which occur already at low dosages. Antiacidic agents do not have a healing effect. Their therapeutical effect is limited only to a pain-reducing component which, with regard to ulcus duodeni, is doubted according to recent experiments (see Blum). Derivatives of glycyrrhetinic acid are known to have a therapeutic effect on ulcers. Yet, serious side-effects, such as aldosterone-like effects, causing a loss of potassium and sodium- and water-retention, strongly limit the possibility of a wider utilization of these derivatives. Psychopharmacological agents have not succeeded in the treatment of ulcers due to a lack of activity. Furthermore, their effects on the central nervous system, such as sedation and influence of motility, are undesirable in ambulatory treatment.